4.6 Article

Discovery and synthesis of 1,2,4-oxadiazole derivatives as novel inhibitors of Zika, dengue, Japanese encephalitis, and classical swine fever virus infections

期刊

ARCHIVES OF PHARMACAL RESEARCH
卷 45, 期 4, 页码 280-293

出版社

PHARMACEUTICAL SOC KOREA
DOI: 10.1007/s12272-022-01380-8

关键词

Antiviral activity; 1; 2; 4-Oxadiazole derivatives; Zika virus; Dengue virus; Japanese encephalitis virus; Classical swine fever virus

资金

  1. Korea Disease Control and Prevention Agency [2018-ER53001-00]
  2. KRICT [KK1703-E00, KK1803-E00, KK1931-20, SI2132-20, SI2232-20]
  3. City University of Hong Kong, Hong Kong SAR, China

向作者/读者索取更多资源

A series of 1,2,4-oxadiazole derivatives with antiviral activity against Zika virus (ZIKV) infection were identified and 28 new compounds were designed, synthesized, and evaluated. Among these compounds, 4-(5-phenyl-1,2,4-oxadiazol-3-yl)-N-(pyridin-3-ylmethyl)aniline showed potent antiviral activity against ZIKV infections and also exhibited activity against other viruses of the Flaviviridae family.
Zika virus (ZIKV), an arbovirus of the Flaviviridae family, has emerged as a significant public health concern owing to its association with congenital abnormalities and severe neurological sequelae. Thus, there is an urgent need to develop effective therapeutic approaches to efficiently treat ZIKV infections. This study used phenotypic screening to identify a series of 1,2,4-oxadiazole derivatives that possess antiviral activity against ZIKV infection. Subsequently, 28 new derivatives were designed, synthesized, and evaluated for this purpose. Among these compounds, 4-(5-phenyl-1,2,4-oxadiazol-3-yl)-N-(pyridin-3-ylmethyl)aniline (5d) had potent antiviral activity against ZIKV infections. Furthermore, a structure-activity relationship analysis indicated that a benzyl substitution on the aniline nitrogen of this compound improved potency while augmenting its drug-like properties. In addition, 5d exhibited antiviral activity against various viruses of Flaviviridae family of worldwide public health importance, such as dengue, Japanese encephalitis and classical swine fever viruses, indicating its potential as a lead compound for generating 1,2,4-oxadiazole derivatives with broad-spectrum anti-flaviviral properties.

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